Patent EA-003274-B1 (EA)
Title: Oxazolidinones as an active substance to treat eye infections
Inventor: COCHRAN ROBERT
IPC: A61K9/06
Filed: 1999-07-07
Abstract: 1. Use of an oxazolidinone selected from: (S)-N-[[3-[3-fluoro-4-[4-(hydroxyacetyl)-1-piperazinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide, (S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide, N-((5S)-3-(3-fluoro-4-(4-(2-fluoroethyl)-3-oxopiperazin-1-yl)phenyl)-2-oxooxazolidin-5-ylmethyl)acetamide, (S)-N-[[3-[5-(3-pyridyl)thiophen-2-yl]-2-oxo-5-oxazolidinyl]methyl]acetamide; and (S)-N-[[3-[5-(4-pyridyl)pyrid-2-yl]-2-oxo-5-oxazolidinyl]methyl]acetamide hydrochloride, for the manufacture of a medicament for administration directly to the eye of a useful warm-blooded mammal, for the treatment of an ophthalmic infection. 2. Use according to claim 1, wherein the mammal is a human. 3. Use according to claim 1, wherein the mammal is a dog or cat. 4. Use according to any preceding claim, wherein the oxazolidinone is: (S)-N-[[3-[3-fluoro-4-[4-(hydroxyacetyl)-1-piperaziny]phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide, or (S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl] acetamide. 5. Use according to claim 4, wherein the oxazolidinone is: (S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide. 6. The use according to any preceding claim, wherein the medicament is a solution, cream, ointment, emulsion, suspension or slow release formulation. 7. Use according to claim 6, wherein the medicament is a solution, cream, ointment, emulsion or suspension. 8. Use according to claim 6, wherein the medicament of a solution in an insert or treatment fluid container. 9. Use according to any preceding claim, wherein the infection is caused by Staphylococcus, Streptococcus, Enterococcus, Bacillus, Corynebacterium, Chlamydia or Neisseria. 10. Use according to claim 9, wherein the infection is caused by Staphylococcus, Streptococcus or Enterococcus. 11. Use according to claim 10, wherein the infection is caused by Staphylococcus or Streptococcus. 12. Use according to any preceding claim, wherein the infection is bacterial keratitis, bacterial conjunctivitis or a corneal ulcer. 13. Use according to claim 12, wherein the infection is bacterial keratitis or bacterial conjunctivitis. 14. A method of treating an ophthalmic infection in a warm-blooded mammal which is in need of such treatment, which comprises administration, directly to the eye of the mammal, of an ophthalmologically effective amount of an oxazolidinone selected from the group consisting of: (S)-N-[[3-[3-fluoro-4-[4-(hydroxyacetyl)-1-piperazinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl] acetamide, (S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide, N-((5S)-3-(3-fluoro-4-(4-(2-fluoroethyl)-3-oxopiperazin-1-yl)phenyl)-2-oxooxazolidin-5-ylmethyl)acetamide, (S)-N-[[3-[5-(3-pyridyl)thiophen-2-yl]-2-oxo-5-oxazolidinyl]methyl]acetamide and (S)-N-[[3-[5-(4-pyridyl)pyrid-2-yl]-2-oxo-5-oxazolidinyl]methyl]acetamide hydrochloride. 15. A method according to claim 14, wherein the useful warm blooded mammal is a human. 16. A method according to claim 14, wherein the useful warm blooded mammal is a dog or cat. 17. A method according to claims 14, wherein the oxazolidinone is selected from the group consisting of: (S)-N-[[3-[3-fluoro-4-[4-(hydroxyacetyl)-1-piperazinyl]-phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide and (S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide. 18. A method according to claim 17, wherein the oxazolidinone is: (S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide. 19. A method according to claim 14, wherein the oxazolidinone is administered in a pharmaceutical formulation selected from the group consisting of a solution, cream, ointment, emulsion, suspension and slow release formulations. 20. A method according to claim 19, wherein the oxazolidinone is administered in a pharmaceutical formulation selected from the group consisting of a solution, cream, ointment, emulsion and suspension. 21. A method according to claim 19, wherein the solution is administered in an insert or treatment fluid container. 22. A method according to claim 14, wherein the oxazolidinone is administered from 2 through 4 times daily. 23. A method according to claim 14, wherein the ophthalmologically effective amount is from 0.3% to 20%. 24. A method according to claim 23, wherein the ophthalmologically effective amount is from 0.5% to 18%. 25. A method according to claim 14, wherein the infection is caused by Staphylococcus, Streptococcus, Enterococcus, Bacillus, Corynebacterium, Chlamydia and Neisseria. 26. A method according to claim 25, wherein the infection is caused by Staphylococcus, Streptococcus and Enterococcus. 27. A method according to claim 25, wherein the infection is caused by Staphylococcus and Streptococcus. 28. A method according to claim 14, wherein the ophthalmic infection is selected from the group consisting of bacterial keratitis, bacterial conjunctivitis and corneal ulcers. 29. The method according to claim 28, wherein the ophthalmic infection is bacterial keratitis and bacterial conjunctivitis.